N-Phenyl-2-pyrimidine-amine Derivatives

Abstract

The present invention relates to novel amides and a process for preparing these amides.

1 . A process for the preparation of a compound of formula IV 
       
         
           
           
               
               
           
         
         wherein R 1 , R 2 , R 4  and R 5  are independently 
         hydrogen, cyano; lower alkyl; hydroxy- or amino-substituted lower alkyl; trifluoromethyl; free, etherified or esterified hydroxy; lower alkoxy; lower alkanoyloxy; free, alkylated or acylated amino; mono- or di-lower alkylamino; lower alkanoylamino; benzoylamino; free or esterified carboxy; lower alkoxycarbonyl and halogen; 
         or 
         R 1  and R 2  or R 4  and R 5  together are a substituted or unsubstituted alkylene radical having 4 carbon atoms, the substituents preferably being selected from cyano, unsubstituted or .hydroxy-, amino- or 4-methyl-piperazinyl-substituted lower alkyl, such as especially methyl, trifluoromethyl, free, etherified or esterified hydroxy, free, alkylated or acylated amino and free or esterified carboxy; 
         R 3  is (4-methyl-piperazinyl)-methyl, 
         R 6 ′ is 4-(3-pyridyl)-2-pyrimidinamino, 
         R 7 ′ is methyl and R 8 ′ is hydrogen, 
         or a pharmaceutically acceptable salt or crystal form thereof, by reacting a compound of formula I 
       
       
         
           
           
               
               
           
         
         wherein R 1  to R 5  are as defined above, R 6  is —NHC(NH)NH 2 , R 7  is methyl and R 8  is hydrogen; 
         with a compound of formula VI 
       
       
         
           
           
               
               
           
         
         wherein R 10  is 3-pyridyl and R 11  is hydrogen or lower alkyl. 
       
     
     
         2 . The process according to  claim 1 , wherein R 11  is methyl. 
     
     
         3 . The process according to  claim 1 , wherein R 1 , R 2 , R 4  and R 5  are all hydrogen. 
     
     
         4 . The process according to  claim 2 , wherein R 1 , R 2 , R 4  and R 5  are all hydrogen.